P
US5322951AExpiredUtilityPatentIndex 72

Certain 1-(2,3-dihydro-indole)carbonyl intermediates

Assignee: BEECHAM GROUP PLCPriority: Jan 5, 1987Filed: Nov 13, 1992Granted: Jun 21, 1994
Est. expiryJan 5, 2007(expired)· nominal 20-yr term from priority
Inventors:KING FRANCIS DJOINER KAREN A
C07D 451/04
72
PatentIndex Score
13
Cited by
1
References
2
Claims

Abstract

An intermediate compound of Formula (V): ##STR1## wherein G is COQ 1 and Q 1 represents chloro, bromo, C 1-4 alkoxy, PhO--, Cl 5 C 6 O--, Cl 3 CO--, succinimidyloxy or imidazolyloxy; the remainder of the terms R 1 , R 2 , R 3 , R 4 , X and Y are defined in the specification. The intermediates of Formula V are useful for preparing 1-(2,3-dihydro-1-carboxamide final products wherein said final products possess 5-HT M-receptor antagonist activity.

Claims

exact text as granted — not AI-modified
We claim: 
     
       1. An intermediate compound of formula (V): ##STR57## wherein G is COQ 1  wherein Q 1  is Chloro, bromo, C 1-4  akoxy, PhO--, Cl 5  C 6  O--, Cl 3  CO--, succinimidyloxy or imidazolyloxy; X and Y are independently selected from hydrogen or C 1-4  alkyl, or together are a bond; R 1  and R 2  are independently selected from hydrogen, C 1-6  alkyl, C 2-6  alkenyl-C 1-4  -alkyl, or together are C 2-4  polymethylene; and R 3  and R 4  are independently selected from hydrogen, halogen, CF 3 , C 1-6  alkyl, C 1-6  alkoxy, C 1-6  alkylthio, C 1-7  -acyl, C 1-7  acylamino, C 1-6  alkylsulphonylamino, N-(C 1-6  alkylsulphonyl)-N-C 1-4  -alkylamino, C 1-6  -alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or Np(aminosulphonyl)-C 1-4  alkylamino optionally N-substituted by one or two groups selected from C 1-6  alkyl, C 3-8  cycloalkyl, C 3-8  cycloalkyl C 1-4  alkyl, phenyl or phenyl C 1-4  alkyl groups or optionally N-disubstituted by C 4-5  polymethylene. 
     
     
       2. An intermediate compound selected from the group consisting of: 1-(2,3-dihydro)-indolyltrichloromethyl carbamate,   1-(2,3-dihydro-3-methyl)indolyl-O-(1-succinimidyl)carbamate,   1-(2,3-dihydro-5-fluoro)indolyl-O-(1-succinimidyl)carbamate,   1-(2,3-dihydro-5-methoxy)indolyl trichloromethyl carbamate,   1-(2,3-dihydro)-indolylcarbonyl chloride,   1-(2,3-dihydro-3-ethyl)indolylcarbonyl chloride,   1-(2,3-dihydro-5-nitro)indolyl-trichloromethyl carbamate,   1-[1-(2,3-dihydro-6-nitro)indolylcarbonyl]-imidazole, and   1-(2,3-dihydro-3,3-dimethyl)indolylcarbonyl chloride.

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